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. Author manuscript; available in PMC: 2021 Mar 1.
Published in final edited form as: Eur J Med Chem. 2020 Jan 2;189:112023. doi: 10.1016/j.ejmech.2019.112023

Table 1.

Amidations of 14a-14c with head group amines to form targeted inhibitors 9 and 18-29 and DOT1L methyltransferase Glo Assay Results.

graphic file with name nihms-1551534-t0012.jpg
product Tail Group
(TG)		 Head Group
(HG)		 Method A
Yield (%)a 		Method B
Yield (%)a 		IC50 ± SD
[μM]b
9 graphic file with name nihms-1551534-t0013.jpg A 25 94 40.8 ± 5.9
18 B 36 80 36.9 ± 1.7
19 C 23 58 69.2 ± 8.0
20 D 28 79 10.9 ± 2.6
21 E 20 66 137.8 ± 17.0
22 graphic file with name nihms-1551534-t0014.jpg A 22 93 23.5 ± 2.7
23 B 18 97 22.4 ± 2.3
24 C 46 83 19.5 ± 0.6
25 D 25 96 1.0 ± 0.1
26 graphic file with name nihms-1551534-t0015.jpg A 17 85 > 100
27 B 16 63 > 100
28 C 25 51 > 100
29 D 18 84 > 100
31 55.6 ± 3.3
IC50 ± SD [nM]b
EPZ004777 0.86 ± 0.1
a

Isolated yields of purified products. Corresponding NMR spectra provided in Supplementary Material.

b

DOT1L methyltransferase-Glo assay.